Preprint Review Version 1 This version not peer reviewed

µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission

Version 1 : Received: 7 September 2017 / Approved: 8 September 2017 / Online: 8 September 2017 (08:22:26 CEST)

A peer-reviewed article of this Preprint also exists.

Tosti, E.; Boni, R.; Gallo, A. µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential. Mar. Drugs 2017, 15, 295. Tosti, E.; Boni, R.; Gallo, A. µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential. Mar. Drugs 2017, 15, 295.

Journal reference: Mar. Drugs 2017, 15, 295
DOI: 10.3390/md15100295

Abstract

The Conus genus includes around 500 species of marine mollusks with a peculiar production of venomous peptides known as conotoxins (CTX). Each species is able to produce up to 200 different biological active peptides. Common structure of CTX is the low number of aminoacids stabilized by disulfide bridges and post-translational modifications that give rise to different isoforms. µ and µ-O CTX are two isoforms that specifically target voltage-gated sodium channels. These, by inducing the entrance of sodium ions in the cell, modulate the neuronal excitability by depolarizing plasma membrane and propagating the action potential. Hyperxcitability and mutations of sodium channels are responsible for perception and transmission of inflammatory and neuropathic pain states. In this review, we describe the current knowledge of µ-CTX interacting with the different sodium channels subtypes, the mechanism of action and their potential therapeutic use as analgesic compounds in the clinical management of pain conditions.

Subject Areas

conotoxin; µ-conotoxin; ion current; sodium channel; pain transmission

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